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Coptis chinensis Franch Directly Inhibits Proteolytic Activation of Kallikrein 5 and Cathelicidin Associated with Rosacea in Epidermal Keratinocytes

1
Biospectrum Life Science Institute, Yongin 16827, Korea
2
Department of Integrative Biotechnology, College of Biotechnology and Bioengineering, Sungkyunkwan University, Suwon 16419, Korea
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(23), 5556; https://doi.org/10.3390/molecules25235556
Received: 14 October 2020 / Revised: 17 November 2020 / Accepted: 25 November 2020 / Published: 26 November 2020
Rosacea is a common and chronic inflammatory skin disease that is characterized by dysfunction of the immune and vascular system. The excessive production and activation of kallikerin 5 (KLK5) and cathelicidin have been implicated in the pathogenesis of rosacea. Coptis chinensis Franch (CC) has been used as a medicinal herb in traditional oriental medicine. However, little is known about the efficacy and mechanism of action of CC in rosacea. In this study, we evaluate the effect of CC and its molecular mechanism on rosacea in human epidermal keratinocytes. CC has the capacity to downregulate the expression of KLK5 and cathelicidin, and also inhibits KLK5 protease activity, which leads to reduced processing of inactive cathelicidin into active LL-37. It was determined that CC ameliorates the expression of pro-inflammatory cytokines through the inhibition of LL-37 processing. In addition, it was confirmed that chitin, an exoskeleton of Demodex mites, mediates an immune response through TLR2 activation, and CC inhibits TLR2 expression and downstream signal transduction. Furthermore, CC was shown to inhibit the proliferation of human microvascular endothelial cells induced by LL-37, the cause of erythematous rosacea. These results demonstrate that CC improved rosacea by regulating the immune response and angiogenesis, and revealed its mechanism of action, indicating that CC may be a useful therapeutic agent for rosacea. View Full-Text
Keywords: rosacea; Coptis chienesis; kallikrein 5; cathelicidin; 1,25 (OH)2VD3; Demodex rosacea; Coptis chienesis; kallikrein 5; cathelicidin; 1,25 (OH)2VD3; Demodex
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MDPI and ACS Style

Roh, K.-B.; Ryu, D.-H.; Cho, E.; Weon, J.B.; Park, D.; Kweon, D.-H.; Jung, E. Coptis chinensis Franch Directly Inhibits Proteolytic Activation of Kallikrein 5 and Cathelicidin Associated with Rosacea in Epidermal Keratinocytes. Molecules 2020, 25, 5556. https://doi.org/10.3390/molecules25235556

AMA Style

Roh K-B, Ryu D-H, Cho E, Weon JB, Park D, Kweon D-H, Jung E. Coptis chinensis Franch Directly Inhibits Proteolytic Activation of Kallikrein 5 and Cathelicidin Associated with Rosacea in Epidermal Keratinocytes. Molecules. 2020; 25(23):5556. https://doi.org/10.3390/molecules25235556

Chicago/Turabian Style

Roh, Kyung-Baeg, De-Hun Ryu, Eunae Cho, Jin B. Weon, Deokhoon Park, Dae-Hyuk Kweon, and Eunsun Jung. 2020. "Coptis chinensis Franch Directly Inhibits Proteolytic Activation of Kallikrein 5 and Cathelicidin Associated with Rosacea in Epidermal Keratinocytes" Molecules 25, no. 23: 5556. https://doi.org/10.3390/molecules25235556

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